中国药房2013，Vol.24Issue(1)：47-48,2.DOI:10.6039/j.issn.1001-0408.2013.01.16
卡巴他赛关键中间体7β,10β-二甲氧基-10-脱乙酰巴卡汀Ⅲ的合成新方法
New Synthesis Method of 7β, 10β-Dimethoxy-10-deacetoxybaccatin Ⅲ as Key Intermediate of Cabazitaxel
摘要
Abstract
OBJECTIVE: To synthesize key intermediate of cabazitaxel, i.e. 7β, 10β-dimethoxy-10-deacetoxybaccatin III with a new method. METHODS: At first, the C(7) and C(10) hydroxy of 10-deacetoxybaccatin III selectively protected; and then, the C(13) hydroxyl was protected by an another reagent. After the deprotection of C(7) and C(10) aydroxyl, the methyla-tion was carried on C(7) and C(10). 7β, 10β-dimethoxy- 10-deacetoxybaccatin Iff was obtained after the deprotection of C(13) hydroxyl, which was characterized by 1H-NMR. RESULTS: 7β, 10β-dimethoxy- 10-deacetoxybaccatin Iff was synthesized successfully with 5 steps of reactions, with purity of 95% and yield of 97%. CONCLUSION: The method will benefit from the good yield, mild conditions and convenient operations, which is suitable for industrial production.关键词
卡巴他赛/中间体/合成/甲基化Key words
Cabazitaxel/ Intermediate/ Synthesis/ Methylation分类
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夏彪,邵波,杨巧宾,李勤耕..卡巴他赛关键中间体7β,10β-二甲氧基-10-脱乙酰巴卡汀Ⅲ的合成新方法[J].中国药房,2013,24(1):47-48,2.
